The protagonist of the present invention, 3-amino-8-(1-piperazinyl)-2H-1-benzo-pyran-2-one, is known as its hydrochloric acid salt. As such it is described as ‘example 8’ in EP 0650 964. Despite the fact that the synthetic route as outlined in said patent has quite an acceptable yield, it is definitely not suited for synthesis on the scale required for a drug in clinical development, let alone the scale required for a marketed drug. The problems with the original synthesis are manifold. First, the key starting material, 3-nitro-2-hydroxybenzaldehyde is not available on a commercial scale, and was prepared by nitration of 2-hydroxybenzaldehyde, resulting in a mixture of 3- and 5-nitro-2-hydroxybenzaldehyde which can only be separated by relatively complicated chromatographic methods. The second step, an Erlenmeyer condensation, results in a very viscous mixture which is hard to stir on a technical scale, and from which the isolation of the desired product appeared difficult as well. The third step, the reduction of the nitro group to the amine, using Fe/HCl is laborious, and the isolation of the reaction product from the large amount of rust (Fe2O3) appeared to be next to impossible on a technical scale. In step 4 the potential carcinogen N-benzyl-bis-chloroethylamine was used. Large scale use of such compounds creates insurmountable safety hazards. After acidic amide hydrolysis (step 5) the end product is contained in a large amount of a mixture of acetic and sulphuric acid. This mixture was neutralized using solid sodium bicarbonate, a laborious task. After the isolation, the crude product had to be purified by chromatography, because the acidic hydrolysis produced a structurally closely related 3-hydroxycoumarin derivative as byproduct. In conclusion: all reaction steps of the synthetic route as outlined in EP 0650 964 show major problems when translated into a pilot scale production of several kilograms of the compound.